This invention relates to 1-carba(1-dethia)cephalosporin antibiotics, intermediates for the preparation thereof, to pharmaceutical formulations comprising the antibiotics, and to a method for the treatment of infectious diseases in man and animals.
The preparation of 1-carbacephalosporins and C-3 substituted methyl derivatives thereof is taught broadly by Christensen et al., in U.S. Pat. No. 4,226,866. Hirata et al., in U.K. patent application No. 2041923, teach a method for preparing 3-H and 3-halo 1-carbacephalosporins, while Hatanaka et al., Tetrahedron Letters, 24, 4837-4838 (1983), teach a method for preparing a 3-hydroxy-(.+-.)-1-carbacephalosporin. A variety of 3-hydroxy-1-carbacephalosporins are also provided in EPO Patent Application Publication 209,352 while their 3-triflate (3-trifluoromethanesulfonic acid) esters are disclosed in EPO Patent Application Publication 211,540.
Takaya in U.K. patent application No. 2043644A discloses 3-phosphonocephalosporanic acid derivatives. Nishide et al. in Chem. Pharm. Bull., 36, 2354-2361 (1988), teaches the synthesis of 3-dialkoxyphosphinylmethyl and 3-dihydroxyphosphinylmethyl cephalosporins.
Although many safe and potent antibiotics of the .beta.-lactam class are known and used clinically, the research into this class of compounds continues in an effort to find antibiotics with improved efficacy, particularly against microorganisms insensitive or resistant to the known antibiotics.